JNJ-10198409 (JNJ10198409)是可口服的、ATP竞争性的血小板衍生生长因子受体酪氨酸激酶PDGF-RTK抑制剂，IC₅₀为2 nM，具有抗血管生成和抗肿瘤活性。JNJ-10198409可以抑制PDGFRα/β活性，IC₅₀为45和4.2 nM。PDGF是一种普遍存在的有丝分裂原，参与调节细胞生长和分裂、胚胎发育、细胞增殖、细胞迁移和血管生成。PDGF的过度表达与动脉粥样硬化、纤维化疾病和恶性肿瘤等多种疾病有关。

参考文献

1.D'Andrea MR, et al. Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis. Mol Cancer Ther. 2005 Aug;4(8):1198-204.

2.Ho CY, et al. (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. J Med Chem. 2005 Dec 29;48(26):8163-73.

冰袋运输。粉末直接保存于-20℃，有效期3年。建议分装后-20℃干燥保存，避免反复冻融。